The chemokine stromal-derived factor-1alpha (SDF-1alpha, CXCL12) and its receptor CXCR4 are implicated in cancer metastasis and inflammation. Weiss & Jacobson, Bioorg Med Chem, 2009, 17(4): 1486-93 and Misra et al, Nucl Med, 2008, 49(6):963-9. Plerixafor (AMD3100) is a known CXCR4 antagonist that has been approved for the mobilization of hematopoietic stem cells by the U.S. Food and Drug Administration. Jacobsen et al. report labeling AMD3100 with the radioisotope 64Cu. Bioorg Med Chem, 2009, 17(4): 1486-93. Biodistribution of 64Cu-AMD3100 showed accumulation in CXCR4-expressing organs. U.S. Patent Application Publication Numbers 2007/0258893 and 2012/0294803 describe imaging compositions and methods for detection of biological conditions associated with expression of CXCR4 receptors. Other imaging agents that target CXCR4 have been reported. See Nimmagadda et al, Cancer research, 2010, 70(10):3935-44; Liang et al, PLoS ONE, 2012, 7(4):e34038; Hanaoka et al, Nucl Med Biol, 2006, 33(4):489-94; Nishizawa et al, Inter J Cancer, 2010, 127(5):1180-7; Nomura et al, Bioconjug Chem, 2008, 19(9): 1917-20. One of the noteworthy peptidic CXCR4 imaging agent with 68Ga is published in Wester et al, Theranostics, 2015, 5(6):618-30. There remains a need for imaging agents that can provide sensitive and rapid detection of pathological conditions associated with the expression of CXCR4 receptors, in particular of inflammation and cancer metastasis.
Mooring et al. report benzenesulfonamides as CXCR4 inhibitors. Chem Med Chem, 2013, 8(4):622-32. See also U.S. Published Patent Application No. 2013/13849646, WO 2008/109154, WO 2005/042489, and CAS Registry Number 1394738-93-2 and 1646745-83-6.
References cited herein are not an admission of prior art.